1-(substituted)benzyl-5-aminoimidazole-4-carboxamides are potent orally active inhibitors of Trypanosoma cruzi in mice

J C Chabala; V B Waits; T Ikeler; A A Patchett; L Payne; L H Peterson; R A Reamer; K Hoogsteen; M Wyvratt; W L Hanson

doi:10.1007/BF02041250

1-(substituted)benzyl-5-aminoimidazole-4-carboxamides are potent orally active inhibitors of Trypanosoma cruzi in mice

Experientia. 1991 Jan 15;47(1):51-3. doi: 10.1007/BF02041250.

Authors

J C Chabala¹, V B Waits, T Ikeler, A A Patchett, L Payne, L H Peterson, R A Reamer, K Hoogsteen, M Wyvratt, W L Hanson, et al.

Affiliation

¹ Merck Sharp & Dohme Research Laboratories, Rahway, New Jersey 07065.

PMID: 1900244
DOI: 10.1007/BF02041250

Abstract

1-(Substituted)benzyl-5-aminoimidazole-4-carboxamides are potent orally active inhibitors of Trypanosoma cruzi infections in mice. The most active compounds are the 1-(4-chlorobenzyl)- and 1-(3,4-dichlorobenzyl)-analogs (L-153,094 [2] and L-153,153 [4], resp.) which are approximately 7-fold more potent upon oral administration than nifurtimox (Lampit) in suppressing parasite levels in the blood of mice with acute Trypanosoma cruzi infections.

Publication types

Comparative Study
Research Support, Non-U.S. Gov't

MeSH terms

Aminoimidazole Carboxamide / analogs & derivatives*
Aminoimidazole Carboxamide / chemical synthesis
Aminoimidazole Carboxamide / therapeutic use*
Animals
Antiprotozoal Agents / chemical synthesis
Antiprotozoal Agents / therapeutic use*
Chagas Disease / drug therapy*
Computer Simulation
Female
Mice
Mice, Inbred Strains
Models, Molecular
Molecular Conformation
Structure-Activity Relationship
Trypanosoma cruzi

Substances

Antiprotozoal Agents
Aminoimidazole Carboxamide